Rosuvast 20 mg

Rosuvastatin 20 mg

Pharmacology
Mechanism of Action
HMG-CoA reductase inhibitor; inhibits the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase

Absorption
Bioavailability: 20%
Peak plasma time: 3-5 hr

Distribution
Vd: 134 L
Protein bound: 88%

Metabolism
Metabolism: ~10% by hepatic CYP2C9
Metabolites: N-desmethyl, lactone

Elimination
Half-Life, Elimination: 19 hr
Excretion: Feces (90%)

Pharmacogenomics
Hepatic influx and efflux transporters (single-nucleotide polymorphisms [SNPs] within the solute carrier organic anion transporter 1B1 (SLCO1B1) gene, encoding the organic anion transporter polypeptide 1B1 (OATP1B1) influx transporter)
SLCO1B1 (OATP1B1) CC genotype significantly increases AUCs of parent drug and metabolites compared with the CT or TT genotypes
This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations
SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)
Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered, to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism
SLCO1B1 CC genotype is most common in Caucasians and Asians (15%); decrease dose by 50% in people of Asian descent
Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and 16.9-fold higher in CC homozygotes than in TT homozygotes
Genetic testing laboratories

  • Optivia Biotechnology, Inc (http://optiviabio.com)

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Rosuvast 20 mg only for the indication prescribed.